Spectroscopic and cytotoxic studies of losartan complexes.

Use of drug-metal complexes for the treatment of several human diseases has resulted in significant progress in the field of medicinal inorganic chemistry. The current study describes the synthesis and characterization of Cu (II) and Ni (II) complexes of Losartan, an antihypertensive drug. These complexes were evaluated for their cytotoxic activity against four human cancer cell lines; SNB-19, HCT-15, COLO-205 and KB-3-1. Spectroscopic characterization revealed that during complex formation, the metal was bound through the nitrogen atoms of the tetrazole moiety of the losartan molecule. The molecular formulas of copper ([Cu (LS) 2 Cl2].6H2O) and nickel ([Ni (LS) 2Cl2]. H2O) complexes were found to be in agreement with the analytical data obtained through elemental analysis. For both the complexes, metal to ligand ratios of 1:2 were calculated. As revealed by FTIR, UV-Visible, and 1H-NMR studies, both the complexes displayed octahedral geometries. Scanning electron microscopy (SEM) revealed marked changes in the morphology of the complexes, compared to the pure drug. From XRD studies, characteristic crystalline peaks of pure losartan were observed whereas no prominent peaks were observed for its complexes. Complexes were found to be inactive in the cytotoxic activity test performed using SNB-19, HCT-15, COLO-205 and KB-3-1 cell lines.

Synthesis, characterization and enzyme inhibitory activity of new pyrazinamide iron complexes.

The present paper deals with synthesis, characterization and amylase inhibitory activity of pyrazinamide (PYZ) with iron in its both (II) and (III) oxidation states. The synthesized complexes were characterized on the basis of IR, UV, 1H-NMR, 13C-NMR, elemental analysis and SEM. Changes in IR data shows that PYZ form complex with octahedral geometry and binding sites are ring nitrogen and carbonyl group, wherein two sides are satisfied with two chloride ions. SEM images indicate the crystalline state and surface morphology of PYZ and its complexes. Elemental analysis proves the composition of complexes. Pyrazinamide and the complexes showed no significant effect on amylase activity but the activity was inhibited in the presence of ferrous chloride.

Metal complexes of isonicotinylhydrazide and their antitubercular activity.

The development and spreading of Multi Drug Resistant TB strains is hampering endeavours for the control and administration of tuberculosis (TB). The expansion episodes of multi-medication safe strains of Mycobacterium tuberculosis against first and second line antituberculosis drugs on one side and the unfavourable effects of these drugs on the other side has led the enthusiasm of researcher towards the synthesis of metal complexes of various medication. This approach is born with the expectation of finding new antituberculous operators without or least reactions as well as being active against the resistant strains of Mycobacterium tuberculosis. This study concentrates on the screening of five metal complexes of isoniazid (INH) against five Mycobacterium tuberculosis strains. These strains have been confirmed by WHO being active and even proliferating safely even in the presence of pyrazinamide, isoniazid (INH), ethambutol and rifampicin. In this work INH was taken as reference medication. All synthesized complexes and INH were subjected for a month and a half in BACTEC MGIT 960 technique. INH and its Fe (II) complex restrained the development of all bacterial strains for merely two weeks, while the Fe(III), Cu(II), Co (II) and Mn (II) complexes repressed the development five strains for three weeks. Conclusively, the strains utilized in this study were discovered to be more susceptible to the later four complexes than the ligand (INH) drug and its Fe (II) complex. Furthermore, elemental analysis and atomic absorption of all complexes were conducted for the determination of metal to ligand ratio.

Fluconazole and its interaction with metal (II) complexes: SEM, Spectroscopic and antifungal studies.

The human digestive tract contains some 100 trillion cells and thousands of species of micro-organisms may be present as normal flora of this tract as well as other mucocutaneous junctions of the body. Candida specie is the most common organism residing in these areas and can easily invade the internal tissues in cases of loss of host defenses. Modifications of previously existing antifungal agents may provide new options to fight against these species. Inorganic compounds of different antifungals are under investigations. Present study report six complexes of fluconazole with Cu (II)), Fe(II), Cd(II), Co(II), Ni(II) and Mn(II) have been synthesized and characterized by elemental analysis, IR, UV and H-NMR. The elemental analysis and spectroscopic data were found in agreement with the expected values as the metal to ligand value was 1:2 ratios with two chlorides in coordination sphere. The morphology of each complex was studied using scanning electron microscope and compared with fluconazole molecule the flaky-slab rock like particles of pure fluconazole was also observed as reported earlier. However, the complexes of fluconazole were showed different morphology in their micrograph. Fluconazole and its complex derivatives have also been screened in vitro for their antifungal activity against Candida albican and Aspergillus niger by MIC method. The complexes showed varied activity ranging from 2-20%.

Multipathways human health risk assessment of trihalomethane exposure through drinking water.

Life-time human health risk of cancer attributed to trihalomethanes in drinking water in an urban-industrialized area of Karachi (Pakistan) was conducted through multiple pathways of exposure. The extent of cancer risk was compared with USEPA guidelines. Human health cancer risk for total trihalomethanes (TTHMs) through ingestion and dermal routes were estimated in "acceptable-low risk" (≥1.0E-06; ≤5.10E-05), whereas through inhalation route it was estimated under "acceptable-high risk" (≥5.10E-05; ≤1.0E-04) category. However, at some industrial-urban areas cancer risk for CHCl3 were estimated under "unacceptable risk" (≥1.0E-04) through inhalation route.

Antibacterial potential of Calotropis procera (flower) extract against various pathogens.

Increased bacterial resistance towards commonly used antibiotics has become a debated issue all over the world in a last few decades. Due to this, consumer demand towards natural anti-microbial agents is increasing day by day. Natural anti-microbial agents have gained enormous attention as an alternative therapeutic agent in pharmaceutical industry. Current study is an effort to explore and identify a bactericidal potential of various solvent extracts of Calotropis procera flower. Flowers of C. procera were extracted with hexane, butanol, ethyl acetate and aqua to evaluate the antibacterial activity by agar well diffusion method against the various human pathogens. The microorganisms used in this study includes Salmonella typhi, Escherichia coli (O157:H7), Micrococcus luteus KIBGE-IB20 (Gen Bank accession: JQ250612) and methicillin resistant Staphylococcus aureus (MRSA) KIBGE-IB23 (Gen Bank accession: KC465400). Zones of inhibition were observed against all four pathogenic strains. Fraction soluble in hexane showed broad spectrum of inhibition against all the studied pathogens. However, fractions soluble in ethyl acetate inhibited the growth of E. coli, MRSA, and M. luteus. In case of butanol and aqueous extracts only growth of M. luteus was inhibited. Results revealed that the flower extracts of C. procera have a potential to be used as an antibacterial agent against these pathogenic organisms.

Design, Synthesis and Antitubercular Evaluation of Novel Series of Pyrazinecarboxamide Metal Complexes.

The interest in the synthesis of metallic complexes of different drugs to make them more efficient in biological environment of the human body is seen for the last few decades. Wide range of metal complexes are already used in clinical practice which encourages additional research for innovating new metal based drugs, such as metal-mediated antibiotics, anti-parasitic, antiviral, antibacterial, and anticancer compounds. Tuberculosis has been known as one of the most disastrous disease putting burden on health system worldwide. Though the therapeutic agents to combat the disease are well practiced, emergence of multi drug resistant strains makes the treatment strategies more difficult. The following work aims to synthesize copper, ferrous, ferric, cobalt and manganese complexes of renowned anti tuberculosis drug, pyrazinamide (PZ). These compounds were tested for anti-tuberculosis using five multidrug resistant strain of Mycobacterium tuberculosis. For this purpose BACTEC MGIT 960 system was used. The drug PZ was also screened with the synthesized complexes. The two complexes of cobalt and manganese proved potent among all of the compounds tested.

Fluoride concentration in drinking water of Karachi city (Pakistan).

The ground and municipal water supply samples of Karachi city were analyzed for their fluoride contents. The fluoride contents in water samples collected from the subsurface and river sources were found below the WHO recommended value for the general health of the people. However, in some industrial areas the groundwater sample showed higher level of fluoride concentration. Continuous monitoring of water resources and cautious fluoridation is suggested to maintain proper status of fluoride concentration in the drinking water.